Dapagliflozin (2S)-1,2-propanediol hydrate is a potent, selective, orally active hSGLT2 inhibitor with EC50 of 1.12 nM.
Dapagliflozin displays >300-fold selectivity over hSGLT1 (EC50=330 nM), highly selectivity versus GLUT transporters.
Dapagliflozin also is a potent selective inhibitor of rSGLT2 (EC50=3 nM), with 200-fold selectivity versus rSGLT1.
Dapagliflozin significantly improves glucose homeostasis, reduces blood glucose levels in hyperglycemic streptozotocin (STZ) rats.
物理化学性质&存储条件
分子量
502.9823
分子式
C24H35ClO9
外观性状
Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
D-Glucitol, 1,5-anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-, (1S)-, compd. with (2S)-1,2-propanediol, hydrate (1:1:1)
参考文献
1. Meng W, et al. J Med Chem. 2008 Mar 13;51(5):1145-9.
2. Han S, et al. Diabetes. 2008 Jun;57(6):1723-9.
3. Wilson C. Nat Rev Endocrinol. 2010 Oct;6(10):531.
4. Komoroski B, et al. Clin Pharmacol Ther. 2009 May;85(5):513-9.
